BGJ398 (Infigratinib) (Synonyms: Infigratinib, NVP-BGJ398) |
Catalog No.GC10055
One-Click Copy Product Info
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BGJ398 (Infigratinib) is an oral, ATP-competitive pan-FGFR tyrosine kinase inhibitor (FGFR1: IC50 = 0.9nM; FGFR2: IC50 = 1.4nM; FGFR3: IC50 = 1nM; FGFR4: IC50 = 60nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 872511-34-7
Sample solution is provided at 25 µL, 10mM.
BGJ398 (Infigratinib) is an oral, ATP-competitive pan-FGFR tyrosine kinase inhibitor (FGFR1: IC50 = 0.9nM; FGFR2: IC50 = 1.4nM; FGFR3: IC50 = 1nM; FGFR4: IC50 = 60nM) [1]. BGJ398 targets the fibroblast growth factor receptors FGFR1, FGFR2, FGFR3, and FGFR4, thereby blocking signal transduction mediated by these receptors and inhibiting FGFR-dependent tumor cell proliferation and angiogenesis [2-3]. BGJ398 is primarily used to treat dwarfism in children [4].
In SKOV3ip1 cells, the survival rate of cell in spheroid culture was significantly reduced after BGJ398 (0.3125-5µM; 72h) treatment [5]. In UMUC-14 cells, the combination of paclitaxel and BGJ398 (0-10µM; 72h) can produce a synergistic effect in promoting cell apoptosis [6].
In TMK-1 cells xenograft mice model, treatment with BGJ398 (10mg/kg; po; 20d) significantly inhibited tumor growth [7]. In Snu16R‑derived xenograft mice model, knockdown of BAG3 enhances the anti-tumor effect induced by BGJ398 (30mg/kg; po; 4 weeks) [8].
References:
[1]. Guagnano V, Furet P, Spanka C, et al. Discovery of 3-(2, 6-dichloro-3, 5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase[J]. Journal of medicinal chemistry, 2011, 54(20): 7066-7083.
[2]. Szymczyk J, Sluzalska K D, Materla I, et al. FGF/FGFR-dependent molecular mechanisms underlying anti-cancer drug resistance[J]. Cancers, 2021, 13(22): 5796.
[3]. Agrawal S, Maity S, AlRaawi Z, et al. Targeting drugs against fibroblast growth factor (s)-induced cell signaling[J]. Current drug targets, 2021, 22(2): 214-240.
[4]. Högler W, Ward L M. New developments in the management of achondroplasia[J]. Wiener Medizinische Wochenschrift, 2020, 170(5): 104-111.
[5]. Cha H J, Choi J H, Park I C, et al. Selective FGFR inhibitor BGJ398 inhibits phosphorylation of AKT and STAT3 and induces cytotoxicity in sphere-cultured ovarian cancer cells[J]. International Journal of Oncology, 2017, 50(4): 1279-1288.
[6]. Kim S H, Ryu H, Ock C Y, et al. BGJ398, a pan-FGFR inhibitor, overcomes paclitaxel resistance in urothelial carcinoma with FGFR1 overexpression[J]. International journal of molecular sciences, 2018, 19(10): 3164.
[7]. Schmidt K, Moser C, Hellerbrand C, et al. Targeting fibroblast growth factor receptor (FGFR) with BGJ398 in a gastric cancer model[J]. Anticancer Research, 2015, 35(12): 6655-6665.
[8]. Li K, Deng X, Feng G, et al. Knockdown of Bcl-2-associated athanogene-3 can enhance the efficacy of BGJ398 via suppressing migration and inducing apoptosis in gastric cancer[J]. Digestive Diseases and Sciences, 2021, 66(9): 3036-3044.
| Cell experiment [1]: | |
Cell lines | SKOV3ip1 cells |
Preparation Method | To measure cell viability of spheroid cultures, SKOV3ip1 cells (5 × 104) were seeded in ultra-low attachment 24-well plates and incubated overnight. BGJ398 were then added, and the cells were incubated for an additional 72 hours. Cells were harvested from each well and transferred to a regular 24-well plate for an additional 12 hours. Attached, live cells were stained with 0.2% crystal violet solution for 20 minutes with gentle agitation. The stained cells were washed with distilled water. For colorimetric analysis, the crystal violet dye was extracted with 1% SDS/PBS, and absorbance was measured at 570nm using an EMax PLUS microplate reader. |
Reaction Conditions | 0.3125-5µM; 72h |
Applications | The survival rate of SKOV3ip1 cells in spheroid culture was significantly reduced after BGJ398 treatment. |
| Animal experiment [2]: | |
Animal models | TMK-1 cells xenograft mice model |
Preparation Method | Cancer cells (1 × 106) were injected subcutaneously into the right flank of 6- to 8-week-old athymic nude mice. Mice were randomly assigned to either a control or treatment group. When tumors reached approximately 80mm3, BGJ398 (10mg/kg, administered by oral gavage) was initiated. Tumor diameters were measured, and volumes were calculated (width2 × length × 0.5). Tumors were excised, weighed, and processed for subsequent experiments. |
Dosage form | 10mg/kg; po; 20d |
Applications | Treatment with BGJ398 significantly inhibited tumor growth. |
References: | |
| Cas No. | 872511-34-7 | SDF | |
| Synonyms | Infigratinib, NVP-BGJ398 | ||
| Chemical Name | 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-[6-[4-(4-ethylpiperazin-1-yl)anilino]pyrimidin-4-yl]-1-methylurea | ||
| Canonical SMILES | CCN1CCN(CC1)C2=CC=C(C=C2)NC3=CC(=NC=N3)N(C)C(=O)NC4=C(C(=CC(=C4Cl)OC)OC)Cl | ||
| Formula | C26H31Cl2N7O3 | M.Wt | 560.48 |
| Solubility | ≥ 7mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7842 mL | 8.9209 mL | 17.8418 mL |
| 5 mM | 356.8 μL | 1.7842 mL | 3.5684 mL |
| 10 mM | 178.4 μL | 892.1 μL | 1.7842 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)